METRITE 500

Indications

• Allergic reactions
• Asthma
• Autoimmune disorders (e.g., lupus, rheumatoid arthritis)
• Multiple sclerosis exacerbations
• Certain types of cancer (e.g., lymphomas)
• Dermatological conditions (e.g., dermatitis, psoriasis)
• Organ transplant rejection prophylaxis

Dosage

Children: Refer to the BNF for Children for specific pediatric dosing recommendations, as doses may vary based on the child's weight and the condition being treated.

Adults: Refer to the BNF for specific dosing guidelines based on the condition being treated. Dosing may vary widely depending on the severity of the condition and the clinical response.

Mechanism of action

Methylprednisolone acts by binding to glucocorticoid receptors in the cytoplasm of target cells, leading to the translocation of the receptor-ligand complex into the nucleus. Once in the nucleus, it regulates gene expression, resulting in the decreased synthesis of inflammatory cytokines and the inhibition of immune cell function. This mechanism contributes to its anti-inflammatory and immunosuppressive effects.

Pharmacodynamics

Methylprednisolone exhibits potent anti-inflammatory effects, which are mediated through the inhibition of leukocyte infiltration at the site of inflammation, as well as the suppression of humoral immune responses and the reduction of the production of pro-inflammatory mediators. Its pharmacodynamic effects can vary based on the dose and duration of treatment.

Pharmacokinetics

Methylprednisolone is well absorbed after oral administration, with a bioavailability of approximately 70-80%. It is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme system, and has a half-life of about 18 to 36 hours, depending on the route of administration. The drug is excreted primarily in urine as metabolites, with only a small fraction eliminated unchanged.

Contra-indications

• Systemic fungal infections
• Hypersensitivity to methylprednisolone or any component of the formulation
• Administration of live or live attenuated vaccines in immunocompromised patients

Adverse effects

• Increased risk of infections
• Gastrointestinal disturbances (nausea, vomiting, peptic ulcer)
• Fluid retention and hypertension
• Hyperglycemia and diabetes
• Osteoporosis and fractures
• Mood changes and psychiatric effects
• Skin changes (thinning, bruising)
• Cushingoid appearance

Interactions

• Nonsteroidal anti-inflammatory drugs (NSAIDs) - increased risk of gastrointestinal bleeding
• Anticoagulants - may alter anticoagulant effects
• Antidiabetic medications - may require adjustment due to hyperglycemic effects
• Live vaccines - may reduce efficacy of vaccines

Precautions

• Use with caution in patients with diabetes, hypertension, or heart disease
• Monitor for signs of infection
• Tapering of dose may be necessary to avoid adrenal suppression
• Long-term use may lead to adrenal insufficiency

Pregnancy

Methylprednisolone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Long-term use during pregnancy may affect fetal development.

Breast-feeding

Methylprednisolone is excreted in breast milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Do not freeze.

Formulations

• Oral tablets
• Injectable solution
• Intravenous formulation